| Structural highlights
Publication Abstract from PubMed
Starting from a series of ureas that were determined to be mechanism-based inhibitors of FAAH, several spirocyclic ureas and lactams were designed and synthesized. These efforts identified a series of novel, noncovalent FAAH inhibitors with in vitro potency comparable to known covalent FAAH inhibitors. The mechanism of action for these compounds was determined through a combination of SAR and co-crystallography with rat FAAH.
Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.,Gustin DJ, Ma Z, Min X, Li Y, Hedberg C, Guimaraes C, Porter AC, Lindstrom M, Lester-Zeiner D, Xu G, Carlson TJ, Xiao S, Meleza C, Connors R, Wang Z, Kayser F Bioorg Med Chem Lett. 2011 Apr 15;21(8):2492-6. Epub 2011 Feb 17. PMID:21392988[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Gustin DJ, Ma Z, Min X, Li Y, Hedberg C, Guimaraes C, Porter AC, Lindstrom M, Lester-Zeiner D, Xu G, Carlson TJ, Xiao S, Meleza C, Connors R, Wang Z, Kayser F. Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2492-6. Epub 2011 Feb 17. PMID:21392988 doi:10.1016/j.bmcl.2011.02.052
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